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dc.contributor.advisor Poka, M. Mongalo, Sello Herlot
dc.contributor.other Demana, M. 2022-09-09T09:38:56Z 2022-09-09T09:38:56Z 2022
dc.description Thesis (M. Pharmacy ((Pharmaceutics)) -- University of Limpopo, 2022 en_US
dc.description.abstract According to the biopharmaceutical classification system, Clarithromycin is considered a class II molecule with low solubility. Poorly soluble drugs result in low bioavailability. Various techniques have been studied to improve the solubility of drugs and subsequently bioavailability. Of these techniques, preparation of amorphous form is the preferred method because it is a more effortless and convenient way to improve the aqueous solubility and dissolution of poorly water soluble drugs. The only disadvantage of amorphous materials is that they are less thermodynamically stable and can recrystallize during processing and storage. Aim: The aim of this study is to prepare amorphous form of clarithromycin to improve its solubility, dissolution rate, and, subsequently, bioavailability. Methods: In this study, preparation of amorphous form of clarithromycin was conducted using the quench cooling method in which the purchased anhydrous crystalline clarithromycin was spread on an aluminum foil and heated to a melting point (217˚C - 220˚C) and then rapidly cooled. Various techniques were conducted to characterize the prepared amorphous clarithromycin, and these include Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), and X-Ray Powder Diffraction (XRPD). In addition, tablets were formulated using the amorphous clarithromycin mixed with selected excipients from compatibility studies, and in vitro dissolution and stability studies were conducted over a period of 6 months. Results: The DSC thermogram results confirmed that the material prepared using the quench cooling process is an amorphous solid-state. Furthermore, the XRPD confirmed an amorphous solid-state with scattering halo peaks. The FTIR also depicted some broader and lower intensity peaks that indicated a formation of an amorphous material. The dissolution rate of amorphous clarithromycin tablets improved by more than 30% when compared to commercial crystalline clarithromycin tablets. The study revealed a drop in dissolution rate at months 3 to 6 under accelerated conditions due to recrystallization. The 6 monthly stability study at long term conditions showed no change in the integrity of the tablets and their contents. Conclusion: As indicated by the study, it can be concluded that the amorphous clarithromycin remained stable during processing and storage under long-term stability for 6 months. Furthermore, based on dissolution results, it can be concluded that amorphous solids have an improved dissolution rate. en_US
dc.description.sponsorship Medical Research Council CHIETA en_US
dc.format.extent xiii, 90 leaves en_US
dc.language.iso en en_US
dc.relation.requires PDF en_US
dc.subject Clarithromycin en_US
dc.subject Amorphous en_US
dc.subject Stability en_US
dc.subject Dissolution en_US
dc.subject Solution-mediated en_US
dc.subject Phase transformation en_US
dc.subject Pharmaceutics en_US
dc.subject.lcsh Amorphous substances en_US
dc.subject.lcsh Solubility en_US
dc.subject.lcsh Solid dosage forms en_US
dc.subject.lcsh Drugs -- Solubility -- Testing en_US
dc.title Formulation and evaluation of amorphous clarithromycin tablets for enhanced dissolution en_US
dc.type Thesis en_US

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